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Gene | FGFR1 |
Variant | V561M |
Impact List | missense |
Protein Effect | gain of function |
Gene Variant Descriptions | FGFR1 V561M lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). V561M results in increased Fgfr1 autophosphorylation and has been shown to be associated with resistance to tyrosine kinase inhibitors (PMID: 25686244, PMID: 15157880, PMID: 28646488), and leads to increased Stat3 phosphorylation and STAT3-dependent gene expression, elevated expression of mesenchymal genes, and increased cell proliferation, migration, and anchorage-independent growth in culture (PMID: 30257990). |
Associated Drug Resistance | Y |
Category Variants Paths |
FGFR1 mutant FGFR1 act mut FGFR1 V561M |
Transcript | NM_023110.3 |
gDNA | chr8:g.38416043C>T |
cDNA | c.1681G>A |
Protein | p.V561M |
Source Database | RefSeq |
Genome Build | GRCh38/hg38 |
Transcript | gDNA | cDNA | Protein | Source Database | Genome Build |
---|---|---|---|---|---|
XM_006716304.2 | chr8:g.38416043C>T | c.1681G>A | p.V561M | RefSeq | GRCh38/hg38 |
XM_017013221 | chr8:g.38416043C>T | c.1681G>A | p.V561M | RefSeq | GRCh38/hg38 |
XM_006716303.4 | chr8:g.38416043C>T | c.1681G>A | p.V561M | RefSeq | GRCh38/hg38 |
NM_023110 | chr8:g.38416043C>T | c.1681G>A | p.V561M | RefSeq | GRCh38/hg38 |
XM_006716304 | chr8:g.38416043C>T | c.1681G>A | p.V561M | RefSeq | GRCh38/hg38 |
XM_017013221.2 | chr8:g.38416043C>T | c.1681G>A | p.V561M | RefSeq | GRCh38/hg38 |
XM_006716304.1 | chr8:g.38416043C>T | c.1681G>A | p.V561M | RefSeq | GRCh38/hg38 |
NM_023110.2 | chr8:g.38416043C>T | c.1681G>A | p.V561M | RefSeq | GRCh38/hg38 |
XM_006716303.3 | chr8:g.38416043C>T | c.1681G>A | p.V561M | RefSeq | GRCh38/hg38 |
XM_017013221.1 | chr8:g.38416043C>T | c.1681G>A | p.V561M | RefSeq | GRCh38/hg38 |
XM_006716303 | chr8:g.38416043C>T | c.1681G>A | p.V561M | RefSeq | GRCh38/hg38 |
NM_023110.3 | chr8:g.38416043C>T | c.1681G>A | p.V561M | RefSeq | GRCh38/hg38 |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
FGFR1 V561M | lung non-small cell carcinoma | resistant | Fexagratinib | Preclinical - Cell culture | Actionable | In a preclinical study, non-small cell lung cancer cells expressing FGFR1 V561M demonstrated resistance to AZD4547 in culture (PMID: 30257990). | 30257990 |
FGFR1 V561M | Advanced Solid Tumor | predicted - resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with Truseltiq (infigratinib) failed to inhibit cell growth and Fgfr1 downstream signaling in cells expressing FGFR1 V561M in culture (PMID: 34114373). | 34114373 |
FGFR1 V561M | Advanced Solid Tumor | predicted - resistant | Ponatinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 V561M demonstrated insensitivity to Iclusig (ponatinib) in culture (PMID: 34114373). | 34114373 |
FGFR1 V561M | Advanced Solid Tumor | predicted - resistant | Erdafitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 V561M demonstrated insensitivity to Balversa (erdafitinib) in culture (PMID: 34114373). | 34114373 |
FGFR1 V561M | Advanced Solid Tumor | predicted - resistant | Futibatinib | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with Lytgobi (futibatinib) failed to inhibit cell growth and Fgfr1 downstream signaling in cells expressing FGFR1 V561M in culture (PMID: 34114373). | 34114373 |
FGFR1 V561M | Advanced Solid Tumor | sensitive | FIIN-1 | Preclinical - Biochemical | Actionable | In a preclinical study, FIIN-1 inhibited Fgfr1 autophosphorylation in a human transformed embryonic kidney cell line harboring FGFR1 V561M mutation in culture (PMID: 20338520). | 20338520 |
FGFR1 V561M | Advanced Solid Tumor | sensitive | PRN1371 | Preclinical - Cell culture | Actionable | In a preclinical study, PRN1371 inhibited proliferation of transformed cells over expressing FGFR1 V561M in culture (PMID: 28978721). | 28978721 |
FGFR1 V561M | Advanced Solid Tumor | predicted - resistant | Pemigatinib | Preclinical - Biochemical | Actionable | In a preclinical study, a cell line expressing FGFR1 V561M was resistant to Pemazyre (pemigatinib) in a kinase assay (PMID: 36698015). | 36698015 |
FGFR1 V561M | Advanced Solid Tumor | predicted - resistant | Pemigatinib | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with Pemazyre (pemigatinib) failed to inhibit cell growth and Fgfr1 downstream signaling in cells expressing FGFR1 V561M in culture (PMID: 34114373). | 34114373 |
FGFR1 V561M | Advanced Solid Tumor | sensitive | Olverembatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Olverembatinib (HQP1351) treatment inhibited cell growth and Fgfr1 phosphorylation and downstream pathway activation in cells expressing FGFR1 V561M in culture and inhibited tumor growth in cell line xenograft models, with a tumor growth inhibition of 49.8% (PMID: 34114373). | 34114373 |
FGFR1 V561M | Advanced Solid Tumor | predicted - sensitive | 3D185 | Preclinical - Biochemical | Actionable | In a preclinical study, 3D185 inhibited kinase activity of FGFR1 V561M in an in vitro assay (PMID: 31438996). | 31438996 |